生物活性
SB225002是趋化因子受体CXCR2高校选择性抑制剂，IC50值为22nM，对CXCR1及其他7-TMRs跨膜受体抑制力弱或无。SB225002 inhibits IL-8- (IC50=8nM) and GROα-mediated (IC50=10nM) calcium mobilisation. SB225002 prevents IL-8-induced neutrophil migration. SB225002 inhibits HIV replication in lymphocytes and macrophages. SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha.
化学数据
| 分子量 | 352.14 |
| 分子式 | C13H10BrN3O4 |
| CAS号 | 182498-32-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 35 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | WHCO1, WHCO5, and WHCO6 cell lines |
| 方法 | Establishing three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally from surgical biopsies of primary esophageal squamous cell carcinomas which are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2.Using the Cell Proliferation kit I to carry out MTT assays . Briefly, plating 1.5 × 103 cells in 96-well plates in a final volume of 180 μL DMEM per well.Adding SB 225002 (antagonist of CXCR2, 400 nM)to cells and adding 0.001% DMSO (solvent) as a control. After the indicated incubation period, adding 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL)to each well and incubating for 4 hours in a humidified atmosphere. Adding one hundred eighty microliters of the solubilization solution to each well and the plates were left overnight at 37°C. Using a microtiter plate reader to measure the spectrophotometric absorbance of samples at 595 nm . |
| 浓度 | 400 nM |
| 处理时间 | 6 days |
| 动物实验 |
|---|
| 动物模型 | Rabbits |
| 配制 | DMSO |
| 剂量 | 5.5 μg/kg/min |
| 给药处理 | Cannula in the external jugular vein |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8398 mL | 14.1989 mL | 28.3978 mL |
| 5 mM | 0.568 mL | 2.8398 mL | 5.6796 mL |
| 10 mM | 0.284 mL | 1.4199 mL | 2.8398 mL |
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